Presented by K.V.

NPAVANKUMAR
CONTENTS :
Introduction
Polymers
Preparation techniques
Drug loading
Drug releasing
Physico chemical characterization
Bio pharmaceuticaI issues
Therapeutic applications
Conclusion
Introduction:
• Nanoparticles are solid colloidal particles ranging
in the size from 10-1000nm in which the active
principle is dissolved entrapped , encapsulated and
or to which the active principle is absorbed and
attached .

• Colloidal dispersion of biodegradable polymer .

•Carry drug molecules to specific organs with in body.

Polymer- based nanoparticulate carriers :
Natural hydrophilic polymers :
• Protein : gelatin , albumin

•Polysaccharides : alginate, dextran , chitosan

•Synthetic hydrophobic polymers :

•Polyesters: poIy(caproIadone) (PECL), PLA, PLGA

Poly(alkylcyanoacrylate) (PACA)
Preparation techniques :
• cross- linking of amphiphilic macromolecules

• Phase separation in an aqueous medium .

• Cross-Iinking in a water-in-oil emulsion.

• Polymerization of acrylic monomers

• Polymer precipitation of hydrophobic

polymer

• Solvent extraction-evaporation

• Solvent displacement or
Nanoprecipitation
Cross- linking of amphiphilic
macromolecules :
cross- linking in a water- in- oil emulsion :
• Protein: HAS , BSA

• Heating temperature higher than 100˚c

• Collect by centrifugation

• Crucial factor for nanosphere production :

emulsification energy and stabilization temperature.

• Chemical cross linking agent : glutaraldehyde.

Preparation of nanoparticles by cross linking in W/O emulsion
technique
AQUEOUS ORGANIC
PHASE PHASE
Protein in Organic solvent /
aqueous oil
phase Surfactant /
suspending agent

EMULSIFICATION
(Sonication , homogenization)
W/O emulsion

Heating / cross linking agent

NANOPARTICLE
Suspension
(external oily phase)
Phase separation in an aqueous
medium :
• By desolvation of the macromolecules.

• By changing in pH or temperature.

• By adding counterions to the aqueous

medium .
 Drug release :
It depends up on following mechanisms ..,

a. Desorption of surface bound drug

b.Diffusion through the nanoparticles

c. Diffusion through the polymer wall .
d. Nanoparticles matrix erosion
i

e. A combined erosion diffusion .

The drug release mechanism , the diffusion

coefficient and the biodegradation rate are the main
factors governing the drug release rate .
Physicochemical characterization :

Size and Morphology

The particle size is one of the most

important parameter of nanoparticles . The main
techniques used to determine the particle size
distribution of nanoparticles includes photon
correlation spectroscopy (pcs) and Electron
microscopy (EM) which measures the individual
particles of size and its distribution .
Surface charge and electrophoretic
mobility:

• Interaction with the biological environment and

electrostatic interaction with bioactive compounds.

•Laser light-scattering technique .

•Surface charge of colloidal particles can be measured
as electrophoretic mobility.
Hydrophobicity of nanoparticle
•Interaction with biological environment (protein
adsorption and cell adhesion).

•Hydrophobicity regulates the extent of

nanoparticles interaction with blood components
Bio pharmaceuticaI issues :
Parenteral administration:
•PACA nanosphere: intracellular cancer therapy.

•Increase ability to penetrate cell membrane.

• Iv administration limitation..,

Up take by MPS: changing the nanospheres’ surface.

• Modulation of distribution pattern: reduction in toxicity

or to prolongation in therapeutic effects .

Subcutaneous and intramuscular
administration :
• Sustained or controlled drug-delivery system

• Residence time was prolonged

• Advantages of nanoparticles over microparticles

Injectability, improved tolerance

• Vaccine adsorbed on to PLA nanoparticles by SC

injection

• Adjuvant effect: small particle size and increase in

hydrophobicity
OraI administration :

• Insulin incorporated into PACA.

•The retarded passage of intact nanocapsules through
rat mucosa and the protection against proteolytic
enzyme in the gut.
OcuIar delivery :

• PACA or PECL nanoparticles.

• Adhere to the ocular epithelial surface .

•Reduction in the systemic side effects.

• Carrier transporting drugs from the lacrymal

fluid toward the inner part of the eye.
Therapeutic applications :
•For intracellular targeting of anti infective drugs to
combat the “ difficulty to treat Intracellular
infections “ of human body.

•For targeting of cytostatic drugs to reduce toxicity

and increase therapeutic activity .

•For specific targeting of anti-inflammatory drugs to

areas of inflammation by which the side effects of
drugs can be minimized .

•For ocular delivery systems .

•To improve the solubility and bioavailability of poorly
soluble drugs .

•To formulate sustain release formulations .

• For targeted delivery of proteins and peptides .

• As adjuvant to vaccines.
Conclusion :

• Nanoparticles are solid , colloidal particles , ranging

from 10-1000nm(1µm) in size.

•As the nanoparticles are prepared from

biodegradable polymers it has less toxic effects .

•By using nanoparticles we can achieve sustained and

control release of drugs.

• Nanoparticles are generally freeze dried (or)

lyophilized for long term conservation of polymeric
nanoparticles.
•Following I.V .administration , nanoparticles under
goes phagocytosis & drug in released.

•Nanoparticles have wide variety of applications in

drug thearpy.